RU2017141446A - ENANTIOMERS OF 2-HYDROXY DERIVATIVE FATTY ACIDS - Google Patents

ENANTIOMERS OF 2-HYDROXY DERIVATIVE FATTY ACIDS Download PDF

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RU2017141446A
RU2017141446A RU2017141446A RU2017141446A RU2017141446A RU 2017141446 A RU2017141446 A RU 2017141446A RU 2017141446 A RU2017141446 A RU 2017141446A RU 2017141446 A RU2017141446 A RU 2017141446A RU 2017141446 A RU2017141446 A RU 2017141446A
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cancer
enantiomer
pharmaceutically acceptable
formula
pathology
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RU2017141446A
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RU2017141446A3 (en
RU2687967C2 (en
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Пабло Висенте ЭСКРИБА РУИС
Мария Лаура МАРТИН
Мария Антония НОГЕРА САЛЬВА
Ксавьер БУСКЕТС КСАУБЕТ
Давид ЛОПЕС ХИМЕНЕС
Майтане ИБАРГУРЕН АЙСПИТАРТЕ
Хосе Хавьер СОТО САЛЬВАДОР
Мигель ИУС АСТИС
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Университат Де Лес Ильес Балеарс
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40Unsaturated compounds
    • C07C59/42Unsaturated compounds containing hydroxy or O-metal groups
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/20Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
    • A61K31/201Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids having one or two double bonds, e.g. oleic, linoleic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/42Separation; Purification; Stabilisation; Use of additives
    • C07C51/487Separation; Purification; Stabilisation; Use of additives by treatment giving rise to chemical modification
    • C07C51/493Separation; Purification; Stabilisation; Use of additives by treatment giving rise to chemical modification whereby carboxylic acid esters are formed
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Oncology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Claims (16)

1. Энантиомер [-] формулы1. Enantiomer [-] of the formula [-]НООС-НОСН-(СН2)6-(СН=СН-СН2)2-(СН2)3-CH3 или его фармацевтически приемлемые соли.[-] HOOC-HOCH- (CH 2 ) 6 - (CH = CH-CH 2 ) 2 - (CH 2 ) 3 -CH 3 or a pharmaceutically acceptable salt thereof. 2. Энантиомер по п. 1, отличающийся тем, что указанный энантиомер представляет собой фармацевтически приемлемую соль формулы2. The enantiomer according to claim 1, characterized in that said enantiomer is a pharmaceutically acceptable salt of the formula [-]NaOOC-НОСН-(СН2)6-(СН=СН-СН2)2-(СН2)3-СН3.[-] NaOOC-HCH - (CH 2 ) 6 - (CH = CH-CH 2 ) 2 - (CH 2 ) 3 -CH 3 . 3. Фармацевтическая композиция для лечения патологии, вызванной аномально низким уровнем сфингомиелина и/или аномально низким уровнем глиофибриллярного кислого белка (ГФКБ) и/или аномально высоким уровнем дигидрофолатредуктазы (ДГФР), содержащая терапевтически эффективное количество энантиомера формулы3. A pharmaceutical composition for treating a pathology caused by an abnormally low level of sphingomyelin and / or an abnormally low level of gliofibrillar acid protein (GFKB) and / or an abnormally high level of dihydrofolate reductase (DHFR), containing a therapeutically effective amount of an enantiomer of the formula [-]НООС-НОСН-(СН2)6-(СН=СН-СН2)2-(СН2)3-CH3 и/или по меньшей мере одной из его фармацевтически приемлемых солей и, необязательно, фармацевтически приемлемый носитель.[-] NOOS-NOSH- (CH 2 ) 6 - (CH = CH-CH 2 ) 2 - (CH 2 ) 3 -CH 3 and / or at least one of its pharmaceutically acceptable salts and, optionally, a pharmaceutically acceptable carrier . 4. Фармацевтическая композиция по п. 3, отличающаяся тем, что указанный энантиомер представляет собой фармацевтически приемлемую соль формулы4. The pharmaceutical composition according to claim 3, characterized in that said enantiomer is a pharmaceutically acceptable salt of the formula [-]NaOOC-НОСН-(СН2)6-(СН=СН-СН2)2-(СН2)3-CH3.[-] NaOOC-LOCCH- (CH 2 ) 6 - (CH = CH-CH 2 ) 2 - (CH 2 ) 3 -CH 3 . 5. Способ лечения патологий, общая этиология которых представляет собой аномально низкий уровень сфингомиелина и/или аномально низкий уровень глиофибриллярного кислого белка (ГФКБ) и/или аномально высокий уровень дигидрофолатредуктазы (ДГФР), включающий введение пациенту терапевтически эффективного количества энантиомера формулы5. A method of treating pathologies whose overall etiology is an abnormally low level of sphingomyelin and / or an abnormally low level of gliofibrillar acid protein (GFKB) and / or an abnormally high level of dihydrofolate reductase (DHFR), comprising administering to the patient a therapeutically effective amount of an enantiomer of the formula [-]НООС-НОСН-(СН2)6-(СН=СН-СН2)2-(СН2)3-СН3 и/или по меньшей мере одной из его фармацевтически приемлемых солей или композиции, содержащей указанный энантиомер и/или по меньшей мере одну из его фармацевтически приемлемых солей.[-] NOOS-NOSH- (CH 2 ) 6 - (CH = CH-CH 2 ) 2 - (CH 2 ) 3 -CH 3 and / or at least one of its pharmaceutically acceptable salts or compositions containing the specified enantiomer and / or at least one of its pharmaceutically acceptable salts. 6. Способ по п. 5, отличающийся тем, что указанный энантиомер представляет собой фармацевтически приемлемую соль формулы6. The method according to p. 5, characterized in that the enantiomer is a pharmaceutically acceptable salt of the formula [-]NaOOC-HOCH-(CH2)6-(CH=CH-CH2)2-(CH2)3-CH3.[-] NaOOC-HOCH- (CH 2 ) 6 - (CH = CH-CH 2 ) 2 - (CH 2 ) 3 -CH 3 . 7. Способ по п. 5, отличающийся тем, что указанная патология, в отношении которой проводят лечение, выбрана из группы, состоящей из рака, сосудистых патологий и метаболических патологий.7. The method according to p. 5, characterized in that the pathology for which treatment is carried out is selected from the group consisting of cancer, vascular pathologies and metabolic pathologies. 8. Способ по п. 7, отличающийся тем, что указанный рак выбран из рака печени, меланомы, рака предстательной железы, рака молочной железы, рака поджелудочной железы, лейкоза, рака шейки матки, рака толстой кишки, рака мозга или рака легких.8. The method according to p. 7, characterized in that said cancer is selected from liver cancer, melanoma, prostate cancer, breast cancer, pancreatic cancer, leukemia, cervical cancer, colon cancer, brain cancer or lung cancer. 9. Способ по п. 7, отличающийся тем, что указанная сосудистая патология выбрана из гипертонии, атеросклероза, кардиомиопатий, ангиогенеза, гиперплазии сердца.9. The method according to p. 7, characterized in that said vascular pathology is selected from hypertension, atherosclerosis, cardiomyopathy, angiogenesis, cardiac hyperplasia. 10. Способ по п. 7, отличающийся тем, что указанная метаболическая патология выбрана из диабета, метаболического синдрома или ожирения.10. The method according to p. 7, characterized in that said metabolic pathology is selected from diabetes, metabolic syndrome or obesity.
RU2017141446A 2011-10-07 2012-10-08 Enantiomers of 2-hydroxy derivatives of fatty acids RU2687967C2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
ES201131622 2011-10-07
ES201131622A ES2401629B1 (en) 2011-10-07 2011-10-07 ENANTIOMERS OF 2-HYDROXIDERIVATES OF FATTY ACIDS AND THEIR USE AS MEDICINES.
US201261610762P 2012-03-14 2012-03-14
US61/610,762 2012-03-14

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RU2017141446A3 RU2017141446A3 (en) 2019-02-13
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JP (1) JP2014530806A (en)
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ES (3) ES2401629B1 (en)
HU (1) HUE035430T2 (en)
IN (1) IN2014CN03111A (en)
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ES2345241B1 (en) * 2009-03-16 2011-09-08 Lipopharma Therapeutics USE OF 2-HYDROXIDERIVATES OF POLYINSATURATED FATTY ACIDS AS MEDICINES.
RU2679443C2 (en) 2014-10-21 2019-02-11 Университат Де Лес Ильес Балеарс Method for synthesis of hydroxy-triglycerides and uses thereof for prevention and treatment of diseases
EP4234035A3 (en) * 2017-05-16 2023-11-15 Ability Pharmaceuticals S.A. A pharmaceutical combination for the treatment of a cancer
WO2019099664A1 (en) * 2017-11-16 2019-05-23 The Research Foundation For The State University Of New York Use of 2-hydroxyoleic acid for the treatment of systemic lupus erythematosus and other immune pathologies
ES2846824B2 (en) * 2020-01-29 2022-01-19 Univ Illes Balears PRODRUGS OF POLYUNSATURATED FATTY ACIDS AND THEIR MEDICAL USES
JP2023518640A (en) * 2020-01-29 2023-05-08 ウニバシタット デ レス イレス バレアース Alpha-hydroxylated fatty acid metabolites, their medical uses and their use as biomarkers
ES2911474B2 (en) * 2020-11-17 2023-02-06 Univ Illes Balears PRODRUGS OF MONOUNSATURATED FATTY ACIDS AND THEIR METABOLITES: MEDICAL USES AND AS BIOMARKERS
MX2022008623A (en) * 2020-02-10 2022-08-08 Ability Pharmaceuticals S L A pharmaceutical combination for the treatment of a cancer.

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RU2235541C2 (en) * 1994-10-04 2004-09-10 Эмори Юниверсити Treatment of atherosclerosis and other cardio-vascular diseases
AUPR547601A0 (en) * 2001-06-05 2001-06-28 Carcraft Qld Pty Ltd Tab with writing surface
ES2186576B1 (en) * 2001-10-11 2004-09-16 Universitat De Les Illes Balears 2-HYDROXYOLEIC ACID TO USE AS A MEDICINAL PRODUCT.
ES2342997B1 (en) * 2008-12-09 2011-06-06 Universitat De Les Illes Balears ALPHA DERIVATIVES OF CIS-MONOINSATURATED FATTY ACIDS TO BE USED AS A MEDICINAL PRODUCT.
ES2345241B1 (en) * 2009-03-16 2011-09-08 Lipopharma Therapeutics USE OF 2-HYDROXIDERIVATES OF POLYINSATURATED FATTY ACIDS AS MEDICINES.

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CN104321300A (en) 2015-01-28
EP3287437B1 (en) 2019-12-11
DK2774910T3 (en) 2018-01-08
RU2017141446A3 (en) 2019-02-13
IN2014CN03111A (en) 2015-07-03
ES2773784T3 (en) 2020-07-14
EP3287437A1 (en) 2018-02-28
EP2774910A1 (en) 2014-09-10
PL2774910T3 (en) 2018-03-30
WO2013050644A1 (en) 2013-04-11
RU2014118123A (en) 2015-11-20
HUE035430T2 (en) 2018-05-02
ES2401629B1 (en) 2014-03-04
US9359281B2 (en) 2016-06-07
JP2014530806A (en) 2014-11-20
US20140288176A1 (en) 2014-09-25
EP2774910B1 (en) 2017-09-27
RU2637937C2 (en) 2017-12-08
PT2774910T (en) 2018-01-03
EP2774910A4 (en) 2015-02-25
ES2653675T3 (en) 2018-02-08
RU2687967C2 (en) 2019-05-17
ES2401629A1 (en) 2013-04-23

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